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RPI-GLYT2-82 | RPI-GLYT2-82 : Non-Competitive/Reversible of SLC6A5
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
SLC6A5
    • IC50:554 ± 80 nM
    up to 5 uM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    off-target Activity (at 10 μM): DAT -22%, Na channel (site 2) -16%, SERT -88%, NET -1.3%, 5-HT2A -7 ...

    Potency
    Cellular
    In Vitro

    SLC6A5

    Mode of Action: Non-Competitive/Reversible

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.5c03329

    In Vivo Validations

    Mouse
    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 1.49 h
    Systemic clearance: 3844 mL/min/Kg
    Area Under the Curve:: 508.6 h·ng/mL
    Volume of Distribution at Steady-State: 7120 mL/Kg

    DOI Reference: 10.1021/acs.jmedchem.5c03329

    Dose: 50 mg/Kg
    Route of delivery: Oral
    Plasma half life: 0.85 h
    Systemic clearance: 3582.8 h·ng/mL
    Cmax: 2701.6 ng/mL
    Tmax: 0.5 h
    Bioavailability: 27.6%

    DOI Reference: 10.1021/acs.jmedchem.5c03329

    Dose: 30 mg/Kg
    Route of delivery: Intraperitoneal
    Plasma half life: 1.08 ± 0.05 h
    Systemic clearance: 2063.72 ± 313.68 mL/min/Kg
    Cmax: 152 ± 31 ng/mL
    Tmax: 1.0 ± 0 h
    Area Under the Curve:: 241 ± 40 h*ng/mL
    Volume of Distribution at Steady-State: 192.93 ± 23.32 L/Kg

    DOI Reference: 10.1038/s41467-026-69616-5

    Chemical Information

    Molecular Formula C24H29N3O3
    SMILEs CN(C)C1(CNC(=O)c2ccc3c(c2)CCN3C(=O)c2ccccc2)CCOCC1
    InChI InChI=1S/C24H29N3O3/c1-26(2)24(11-14-30-15-12-24)17-25-22(28)20-8-9-21-19(16-20)10-13-27(21)23(29)18-6-4-3-5-7-18/h3-9,16H,10-15,17H2,1-2H3,(H,25,28)
    Molecular weight 407.22 Da
    AlogP 2.7301
    HBond acceptors 6
    HBond donors 1
    Atoms 59

    Expert Reviews

    by SERP
    (on 13 May 2026)
    Cellular Use Rating
    In Model Organisms
    The compound was evaluated against 38 potential off-targets and showed significant inhibition on 5HT2A (IC50=1.9 uM, 3.4-fold selectivity) and SERT (IC50=4.7 uM, 8.5-fold selectivity) in cellular functional...
    by SERP
    (on 4 Aug 2026)
    In Model Organisms
    The most supportable synthesis is that GlyT2 is evolutionarily conserved across vertebrates, but species differ in gene structure, isoforms, regional expression, and regulatory control; human data mainly...
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